A Perspective on the Permeability of Cocrystals/Organic Salts of Oral Drugs.

According to the BCS classification system, the differentiation of drugs is based on two essential parameters of solubility and permeability, meaning the latter is as pivotal as the former in creating marketable pharmaceutical products. Nevertheless, the indispensable role of permeability in pharmaceutical cocrystal profiles has not been sufficiently cherished, which can be most probably attributed to two principal reasons. First, responsibility may be on more user-friendly in vitro measurement procedures for solubility compared to permeability, implying the permeability measurement process seems unexpectedly difficult for researchers, whereas they have a complete understanding of solubility concepts and experiments. Besides, it may be ascribed to the undeniable attraction of introducing new crystal-based structures which mostly leaves the importance of improving the function of existing multicomponents behind. Bringing in new crystalline entities, to rephrase it, researchers have a fairly better chance of achieving high-class publications. Although the Food and Drug Administration (FDA) has provided a golden opportunity for pharmaceutical cocrystals to straightforwardly enter the market by simply considering them as derivatives of the existing active pharmaceutical ingredients, inattention to assessing and scaling up permeability which is intimately linked with solubility has resulted in limited numbers of them in the global pharmaceutical market. Casting a glance at the future, it is apprehended that further development in the field of permeability of pharmaceutical cocrystals and organic salts requires a meticulous perception of achievements to date and potentials to come. Thence, this perspective scrutinizes the pathway of permeation assessment making researchers confront their fear upfront through mapping the simplest way of permeability measurement for multicomponents of oral drugs.

Accelerated Wound Healing with a Diminutive Scar through Cocrystal Engineered Curcumin.

Pharmaceutical cocrystals ( Regulatory Classification of Pharmaceutical Co-Crystals Guidance for Industry; Food and Drug Administration, 2018) are crystalline solids produced through supramolecular chemistry to modulate the physicochemical properties of active pharmaceutical ingredients (APIs). Despite their extensive development in interdisciplinary sciences, this is a pioneering study on the efficacy of pharmaceutical cocrystals in wound healing and scar reducing. Curcumin-pyrogallol cocrystal (CUR-PYR) was accordingly cherry-picked since its superior physicochemical properties adequately compensate for limitative drawbacks of curcumin (CUR). CUR-PYR has been synthesized by a liquid-assisted grinding (LAG) method and characterized via FT-IR, DSC, and PXRD analyses. In vitro antibacterial study indicated that CUR-PYR cocrystal, CUR+PYR physical mixture (PM), and PYR are more effective against both Gram-negative (Pseudomonas aeruginosa and Escherichia coli) and Gram-positive (Staphylococcus aureus and Bacillus subtilis) bacteria in comparison with CUR. In vitro results also demonstrated that the viability of HDF and NIH-3T3 cells treated with CUR-PYR were improved more than those received CUR which is attributed to the effect of PYR in the form of cocrystal. The wound healing process has been monitored through a 15 day in vivo experiment on 75 male rats stratified into six groups: five groups treated by CUR-PYR+Vaseline (CUR-PYR.ung), CUR+PYR+Vaseline (CUR+PYR.ung), CUR+Vaseline (CUR.ung), PYR+Vaseline (PYR.ung), and Vaseline (VAS) ointments and a negative control group of 0.9% sodium chloride solution (NS). It was revealed that the wounds under CUR-PYR.ung treatment closed by day 12 postsurgery, while the wounds in other groups failed to reach the complete closure end point until the end of the experiment. Surprisingly, a diminutive scar (3.89 ± 0.97% of initial wound size) was observed in the CUR-PYR.ung treated wounds by day 15 after injury, followed by corresponding values for PYR.ung (12.08 ± 2.75%), CUR+PYR.ung (13.89 ± 5.02%), CUR.ung (16.24 ± 6.39%), VAS (18.97 ± 6.89%), and NS (20.33 ± 5.77%). Besides, investigating histopathological parameters including inflammation, granulation tissue, re-epithelialization, and collagen deposition signified outstandingly higher ability of CUR-PYR cocrystal in wound healing than either of its two constituents separately or their simple PM. It was concluded that desired solubility of the prepared cocrystal was essentially responsible for accelerating wound closure and promoting tissue regeneration which yielded minimal scarring. This prototype research suggests a promising application of pharmaceutical cocrystals for the purpose of wound healing.

Evaluation of gamma ray and neutron attenuation capability of thermoplastic polymers.

The fast neutron and gamma ray attenuation capability of the most common thermoplastic polymers used in nuclear applications has been evaluated theoretically. Monte Carlo simulation has been used to compute the gamma-ray energy absorption buildup factor in the energy range 0.015-15 MeV at penetration depths up to 40 MFP. The results of MCNPX calculations have been validated against the results derived from the Geometric Progression fitting method. To evaluate neutron attenuation performance of the polymers, the fast neutron removal cross-section has been determined using theoretical database. Despite the superior ability of polysulfone and poly (ether sulfone) in gamma ray attenuation, high-density polyethylene has been found to have the best fast neutron removal ability among all. The detailed insights into the fast neutron and gamma ray shielding properties of selected polymers in the present work might have great potential applications in nuclear systems.